Lumitene

Generic Name: Beta Carotene
Class: Vitamin A
ATC Class: A11HA
VA Class: VT050
Molecular Formula: C40H56
CAS Number: 7235-40-7

Introduction

Weak antioxidant; precursor of vitamin A.a e f

Uses for Lumitene

Erythropoietic Protoporphyria

Used to reduce the severity of photosensitivity reactions in patients with erythropoietic protoporphyria (EPP).a e

Increases the development time for minimal erythema in EPP patients exposed to artificial light and sunlight.a

Macular Degeneration

Has been used in high-dose antioxidant supplements containing ascorbic acid and vitamin E with zinc in high-risk patients with age-related macular degeneration.128 130

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Other Photosensitivity Reactions

Has been used in the management of polymorphous light eruption and photosensitivity caused by diseases other than EPP;a further studies are required.a

Other Uses

Not effective as a sunscreen.a f

Not recommended to reduce cardiovascular risk.100 101 102 105 106 107 118 e

Beta carotene supplementation has not been shown to reduce the risk for developing lung or other cancers.e

Lumitene Dosage and Administration

General

Erythropoietic Protoporphyria

  • Adjust dosage according to individual requirements and response.a f Adjust dosage to maintain blood carotene concentrations of 4–6 mcg/mL.a

  • Several weeks of therapy are often required before enough beta carotene has accumulated in the skin to exert a protective effect.a f

  • Patients should not increase time of exposure to the sun until carotenodermia is evident (e.g., yellowness of palms and soles).a f When carotenodermia occurs, cautiously and gradually increase exposure to the sun.a f

Administration

Oral Administration

Administer orally as a single daily dose or in divided doses, preferably with meals.a f h

Contents of capsules may be mixed with orange or tomato juice to facilitate administration to children.a f

Dosage

Dosage expressed in terms of beta carotene; may also be expressed in terms of vitamin A in international units (IU) or retinol equivalents (RE).d f g h

1 IU beta carotene is equivalent to 0.6 mcg beta carotene.g

1 RE is equivalent to 6 mcg of dietary beta carotene.f g

Pediatric Patients

Erythropoietic Protoporphyria
Oral

Children <14 years of age: Usually, 30–150 mg (50,000–250,000 IU beta carotene) daily.a f

Adults

Erythropoietic Protoporphyria
Oral

Usually, 30–300 mg (50,000–500,000 IU beta carotene) daily.a e f

Macular Degeneration
Oral

15 mg daily in combination with ascorbic acid 500 mg daily, vitamin E 400 units daily, and zinc (as zinc oxide) 80 mg daily, with copper (as cupric oxide) 2 mg daily (to prevent anemia).128 130

Special Populations

No special populations dosage recommendations at this time.f

Cautions for Lumitene

Contraindications

  • Known hypersensitivity to beta carotene or any ingredient in the formulation.a f

Warnings/Precautions

Warnings

Lung Cancer

Increased incidence of lung cancer following beta carotene supplementation has been reported in clinical trials of adult smokers and those exposed to asbestos.113 129 e

Carcinogenic potential of beta carotene supplementation has not been determined to date.a However, beta carotene supplementation was not carcinogenic in animal studies.e

Cardiovascular Disease

Beta carotene supplementation may increase cardiovascular risk (e.g., coronary artery disease, cardiovascular mortality), especially in current smokers.101 105 106 e

Sensitivity Reactions

Peanut Hypersensitivity

Some preparations of beta carotene (Lumitene) contain peanut oil.f

General Precautions

Skin Discoloration

Excessive beta carotene ingestion may cause reversible carotenodermia (yellowish skin discoloration); carotenodermia usually disappears when beta carotene is reduced or discontinued.f

Specific Populations

Pregnancy

Category C.b f

Lactation

Not known whether beta carotene is distributed into milk.a f Use with caution.a f

Hepatic Impairment

Safety not established; use with caution.a f

Renal Impairment

Safety not established; use with caution.a f

Common Adverse Effects

Reversible carotenodermia,a e f loose stools.a f

Interactions for Lumitene

Specific Drugs

Drug

Interaction

Comments

Orlistat

May decrease GI absorption of fat-soluble vitamins (e.g., beta carotene)119

Allow at least 2 hours to elapse between (before or after) any orlistat dose and beta carotene administration119 121 125 127

Lumitene Pharmacokinetics

Absorption

Bioavailability

Absorption depends on the presence of bile and absorbable fat in the intestinal tract.a e f

Supplemental forms of beta carotene have markedly greater bioavailability than dietary beta carotene.e

Only 20–30% of supplemental beta carotene is absorbed unchanged.a

Onset

Photosensitivity protecting action occurs after at least 2–4 weeks and usually coincides with the development of carotenodermia.a

Duration

Decreased tolerance to light usually is evident within 1–2 weeks after discontinuing beta carotene therapy.a

Plasma Concentrations

Blood carotene concentrations reach a maximum and carotenodermia usually develops about 4–6 weeks after beginning beta carotene therapy.a

Special Populations

Absorption is greatly decreased in patients with steatorrhea and chronic diarrhea.a

Distribution

Extent

Widely distributed in the body.a e Accumulates in the skin and in various tissues, particularly depot fat.a

Not known if distributed into human milk.a f

Elimination

Metabolism

Metabolized, principally in the small intestine, to vitamin A;a f smaller amounts metabolized in the liver.f

Elimination Route

Excreted in fecesf and urine as metabolites.a

Stability

Storage

Oral

Capsules

Tight, light-resistant containers.a

Actions

  • A carotenoid pigment that occurs naturally in green and yellow vegetables.a f

  • Precise mechanism by which beta carotene exerts photoprotection has not been established;a may quench the formation of singlet excited oxygen.a

  • No effect on the basic biochemical abnormality of EPP (i.e., erythrocyte, plasma, and stool concentrations of protoporphyrins are not altered by the drug).a

Advice to Patients

  • Inform patients that carotenodermia may develop after 2–6 weeks of therapy; usually first noticed as yellowness of the palms of the hands or soles of the feet and to a lesser extent of the face.a f

  • Advise patients against taking supplementary vitamin A because beta carotene will fulfill normal vitamin A requirements.a f

  • Advise EPP patients that the protective effect of beta carotene is not total and that they may still develop considerable burning and edema after sufficient exposure to sunlight.a f Explain that each patient must establish his own time limit of exposure to sunlight.a f

  • Inform EPP patients not to increase time of exposure to the sun until carotenodermia is evident.a f

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.f

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.f

  • Importance of informing patients of other important precautionary information.f (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Beta Carotene

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

15 mg*

30 mg

60 mg*

Lumitene (with peanut oil and methyl and propyl parabens)

Tishcon

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Diaz MN, Frei B, Vita JA et al. Antioxidants and atherosclerotic heart disease. N Engl J Med. 1997; 337:408-16. [IDIS 389182] [PubMed 9241131]

101. Stephens N. Anti-oxidant therapy for ischemic heart disease: where do we stand? Lancet. 1997; 349:1710-1.

102. Rowe PM. Beta-carotene takes a collective beating. Lancet. 1996; 347:249. [PubMed 8551889]

103. Greenberg ER, Baron JA, Karagas MR et al. Mortality associated with low plasma concentration of beta carotene and the effect of oral supplementation. JAMA. 1996; 275:699-703. [IDIS 360965] [PubMed 8594267]

104. Rimm EB, Stampfer MJ, Ascherio A et al. Vitamin E consumption and the risk of coronary heart disease in men. N Engl J Med. 1993; 328:1450-6. [IDIS 314551] [PubMed 8479464]

105. Rapola JM, Virtamo J, Haukka JK et al. Effect of vitamin E and beta carotene on the incidence of angina pectoris: a randomized, double-blind, controlled trial. JAMA. 1996; 275:693-8. [IDIS 360964] [PubMed 8594266]

106. Omenn GS, Goodman GE, Thornquist MD et al. Effects of a combination of beta carotene and vitamin A on lung cancer and cardiovascular disease. N Engl J Med. 1996; 334:1150-5. [IDIS 363829] [PubMed 8602180]

107. Hennekens CH, Buring JE, Manson JE et al. Lack of effect of long-term supplementation with beta carotene on the incidence of malignant neoplasms and cardiovascular disease. N Engl J Med. 1996; 334:1145-6. [IDIS 363828] [PubMed 8602179]

108. Jha P, Flather M, Lonn E et al. The antioxidant vitamins and cardiovascular disease: a critical review of epidemiologic and clinical trial data. Ann Intern Med. 1995; 123:860-72. [IDIS 356628] [PubMed 7486470]

109. Reaven PD, Khouw A, Beltz WF et al. Effect of dietary antioxidant combinations in humans: protection of LDL by vitamin E but not by beta-carotene. Arterioscler Thromb. 1993; 13:590-600. [PubMed 8466894]

110. Jialal I, Norkus EP, Cristol L et al. β-Carotene inhibits the oxidative modification of low-density lipoprotein. Biochim Biophys Acta. 1991; 1086:134-8. [PubMed 1954240]

111. Greenberg ER, Sporn MB. Antioxidant vitamins, cancer, and cardiovascular disease. N Engl J Med. 1996; 334:1189-90. [IDIS 363832] [PubMed 8602188]

112. National Research Council, Committee on Diet and Health, Food and Nutrition Board, Commission on Life Sciences. Diet and health: implications for reducing chronic diseases. Washington, DC: National Academy of Press; 1989.

113. The Alpha-Tocopherol, Beta Carotene Cancer Prevention Study Group. The effect of vitamin E and beta carotene on the incidence of lung cancer and other cancers in male smokers. N Engl J Med. 1994; 330:1029-35. [IDIS 328112] [PubMed 8127329]

114. Blot WJ, Li JY, Taylor PR et al. Nutrition intervention trials in China: supplementation with specific vitamin/mineral combinations, cancer incidence, and disease-specific mortality in the general population. J Natl Cancer Inst. 1993; 85:1483-92. [PubMed 8360931]

115. Blot WJ, Li JY, Taylor PR. Lung cancer and vitamin supplementation. N Engl J Med. 1994; 331:614. [IDIS 334519] [PubMed 8047094]

116. Greenberg ER, Baron JA, Tosteson TR et al for the Polyp Prevention Study Group. A clinical trial of antioxidant vitamins to prevent colorectal adenoma. N Engl J Med. 1994; 331:141-7. [IDIS 332766] [PubMed 8008027]

117. Greenberg ER, Baron JA, Stukel TA et al for the Skin Cancer Prevention Study Group. A clinical trial of beta carotene to prevent basal-cell and squamous-cell cancers of the skin. N Engl J Med. 1996; 323:789-95.

118. Ryan TJ, Antman EM, Brooks NH et al. ACC/AHA guidelines for the management of patients with acute myocardial infarction: 1999 update: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Management of Acute Myocardial Infarction). From ACC website.

119. Roche Laboratories Inc. Xenical (orlistat) capsules prescribing information. Nutley, NJ; 1999 April.

120. Sjöström L, Rissanen A, Andersen T et al. Randomized placebo-controlled trial of orlistat for weight loss and prevention of weight regain in obese patients. Lancet. 1998; 352:167-72. [IDIS 407969] [PubMed 9683204]

121. Davidson MH, Hauptman J, DiGirolamo M et al. Weight control and risk factor reduction in obese subjects treated for 2 years with orlistat. JAMA. 1999; 281:235-42. [IDIS 417495] [PubMed 9918478]

122. Hollander PA, Elbein SC, Hirsch IB et al. Role of orlistat in the treatment of obese patients with type 2 diabetes: a 1-year randomized double-blind study. Diabetes Care. 1998; 21:1288-94. [IDIS 411429] [PubMed 9702435]

123. Melia AT, Koss-Twardy SG, Zhi J. The effect of orlistat, an inhibitor of dietary fat absorption, on the absorption of vitamins A and E in healthy volunteers. J Clin Pharmacol. 1996; 36:647-53. [IDIS 370479] [PubMed 8844448]

124. Zhi J, Melia AT, Koss-Twardy SG et al. The effect of orlistat, an inhibitor of dietary fat absorption, on the pharmacokinetics of β-carotene in healthy volunteers. J Clin Pharmacol. 1996; 36:152-9. [IDIS 364805] [PubMed 8852391]

125. Roche Laboratories Inc. Xenical (orlistat) capsules patient information. Nutley, NJ; 1999 April.

126. James WP, Avenell A, Broom J et al. A one-year trial to assess the value of orlistat in the management of obesity. Int J Obes Relat Metab Disord. 1997; 21(Suppl 3):S24-30. [PubMed 9225173]

127. Roche Laboratories Inc, Nutley, NJ: Personal communication on Orlistat 56:40.

128. Age-Related Eye Disease Study Research Group. A randomized, placebo-controlled, clinical trial of high-dose supplementation with vitamins C and E, beta carotene, and zinc for age-related macular degeneration and vision loss. Arch Ophthalmol. 2001; 119:1417-36. [PubMed 11594942]

129. Omenn GS, Goodman GE, Thornquist MD et al. Effects of a combination of beta carotene and vitamin A on lung cancer and cardiovascular disease. N Engl J Med. 1996; 334:1150-5. [IDIS 363829] [PubMed 8602180]

130. Jampol LM. Antioxidants, zinc, and age-related macular degeneration. Arch Opthalmol. 2001; 119-1533-4. Editorial.

a. AHFS Drug Information 2007. McEvoy GK, ed. Beta carotene. Bethesda, MD: American Society of Health-System Pharmacists; 2007: 3618-9.

b. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation, 7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005:154.

c. Food and Drug Administration. Food Labeling: Health Claims; Antioxidant Vitamin A and Beta-Carotene and the Risk in Adults of Atherosclerosis, Coronary Heart Disease, and Certain Cancers. Final rule. [21 CFR Part 101] Fed Regist. 1998; 63:34092-97.

d. Department of Health and Human Services, Food and Drug Administration. Part 101---Food Labeling. Subpart C---Specific Nutrition Labeling Requirement and Guidelines. Sec 101.36---Nutrition Labeling of dietary supplements. (21 CFR (4-1-03 Ed.)). 2003:79-91.

e. Food and Nutrition Board. Dietary reference intakes for vitamin C, vitamin E, selenium and carotenoids. A report of the Panel on Dietary Antioxidants and Related Compounds. Washington DC, National Academy Press: 2000;25-72.

f. Tishcon Corp. Lumitene (beta carotene) capsules prescribing information. Westbury, NY; Undated.

g. World Health Organization. WHO report on vitamin and mineral requirements in human nutrition. Vitamin A. Geneva; WHO. 2004:17–44.

h. Now Natural Foods. Beta Carotene softgels (25,000 IU as pro-Vitamin A 15 mg, Vitamin E 5 IU and Lecithin 10 mg) product information. Bloomingdale, IL; Undated.

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